Department of Pharmaceutical Sciences, Dr. Harisingh Gour Central University, Sagar, MP, India.
Department of Pharmaceutical Sciences, Dr. Harisingh Gour Central University, Sagar, MP, India; Use-inspired Biomaterials & Integrated Nano Delivery (U-BiND) Systems Laboratory, Department of Pharmaceutical Sciences, Wayne State University, Detroit, MI, USA.
Int J Biol Macromol. 2019 May 1;128:740-751. doi: 10.1016/j.ijbiomac.2019.01.147. Epub 2019 Jan 27.
The current research is focused to develop and investigate the toxicity and penetration potential of biocompatible chitosan nanogel encapsulating capecitabine by ionic interaction mechanism exhibiting pH triggered transdermal targeting. The nanogel (CPNL) was synthesized by ion gelation mechanism using Pluronic F 127 and surface decoration by Transcutol as non-ionic penetration enhancer. The CPNL possesses fine morphology and nano size range when evaluated by TEM, SEM and DLS analysis with cationic charge and slightly acidic pH assayed by zeta potential and pH analysis. It showed pH responsive drug release characteristics mimicking the skin cancer micro-environment. The MTT assay and apoptotic index of CPNL on HaCaT cell line elaborated optimal cell toxicity and retention on 24h of exposure. The ex-vivo skin penetration analysis exhibited noteworthy diffusion and penetration caliber through concentration depth profile, steady state flux and fluorescent skin imaging on porcine tissue. Overall outcomes suggested CPNL as a potent alternative biocompatible, transdermal nanotherapy against skin cancer displaying significant penetration caliber with enhance toxicity on cancerous cell.
当前的研究集中于开发和研究通过离子相互作用机制包封卡培他滨的生物相容性壳聚糖纳米凝胶的毒性和渗透潜力，该机制表现出 pH 触发的透皮靶向性。纳米凝胶（CPNL）通过离子凝胶化机制使用 Pluronic F127 合成，并通过 Transcutol 进行表面修饰作为非离子渗透增强剂。通过 TEM、SEM 和 DLS 分析评估，CPNL 具有精细的形态和纳米尺寸范围，通过zeta 电位和 pH 分析测定具有阳离子电荷和略酸性 pH。它显示出 pH 响应的药物释放特性，模拟皮肤癌微环境。MTT 测定和 CPNL 对 HaCaT 细胞系的凋亡指数详细说明了在暴露 24 小时时最佳的细胞毒性和保留率。离体皮肤渗透分析通过浓度深度分布、稳态通量和猪组织上的荧光皮肤成像显示出显著的扩散和渗透能力。总体结果表明，CPNL 作为一种有效的替代生物相容性、透皮纳米疗法，用于治疗皮肤癌，具有显著的渗透能力，并增强了对癌细胞的毒性。
